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製品番号: HY-164492

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LSN3074753

LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1455031-68-1
分子式: C₂₄H₃₀FN₅O₂
分子量:439.53

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

LSN3074753 構造式

CAS 番号: 1455031-68-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

Raf アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	ED₅₀	1.7 mg/kg Compound: 6	In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed athymic nu/nu mouse assessed as inhibition of ERK phosphorylation by ELISA In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed athymic nu/nu mouse assessed as inhibition of ERK phosphorylation by ELISA	[PMID: 25965804]
A-375	IC₅₀	0.01 μM Compound: 6	Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay	[PMID: 25965804]
A-375	IC₅₀	0.022 μM Compound: 6	Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay	[PMID: 25965804]
HCT-116	IC₅₀	0.16 μM Compound: 6	Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA	[PMID: 25965804]
HCT-116	IC₅₀	0.174 μM Compound: 6	Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay	[PMID: 25965804]

化学情報

CAS 番号 1455031-68-1
分子量 439.53
分子式 C₂₄H₃₀FN₅O₂
SMILES

O=C(NC[C@@H](O)C(C)(C)C)NC1=CC(C2=CC3=CN=C(NC)C=C3N=C2C)=C(C)C=C1F
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (266 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Yao YM, et al. Mouse PDX Trial Suggests Synergy of Concurrent Inhibition of RAF and EGFR in Colorectal Cancer with BRAF or KRAS Mutations. Clin Cancer Res. 2017 Sep 15;23(18):5547-5560. [Content Brief]

[2]. Sorokin A, et al. Antitumor activity of panRAF inhibition in BRAF V600E metastatic colorectal cancer[J]. 2017.

Calculators

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希釈計算機

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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